PMID

Data

Article Title

Organization

Discovery of highly potent, selective, and efficacious small molecule inhibitors of ERK1/2.

Array Biopharma

8-Tetrahydropyran-2-yl chromans: highly selective beta-site amyloid precursor protein cleaving enzyme 1 (BACE1) inhibitors.

Array Biopharma

Discovery of 2-pyridylureas as glucokinase activators.

Array Biopharma

Discovery of 5,6,7,8-tetrahydropyrido[3,4-d]pyrimidine inhibitors of Erk2.

Array Biopharma

Discovery of 7-tetrahydropyran-2-yl chromans:ß-site amyloid precursor protein cleaving enzyme 1 (BACE1) inhibitors that reduce amyloidß-protein (Aß) in the central nervous system.

Array Biopharma

Discovery of a Novel Class of Imidazo[1,2-a]Pyridines with Potent PDGFR Activity and Oral Bioavailability.

Array Biopharma

Identification of a new class of glucokinase activators through structure-based design.

Array Biopharma

Spirocyclicß-site amyloid precursor protein cleaving enzyme 1 (BACE1) inhibitors: from hit to lowering of cerebrospinal fluid (CSF) amyloidß in a higher species.

Array Biopharma

Discovery and preclinical pharmacology of a selective ATP-competitive Akt inhibitor (GDC-0068) for the treatment of human tumors.

Array Biopharma

Non-charged thiamine analogs as inhibitors of enzyme transketolase.

Array Biopharma

Synthesis, in vitro and in vivo activity of thiamine antagonist transketolase inhibitors.

Array Biopharma

Non-oxime pyrazole based inhibitors of B-Raf kinase.

Array Biopharma

Discovery of spirocyclic sulfonamides as potent Akt inhibitors with exquisite selectivity against PKA.

Array Biopharma

Discovery and SAR of spirochromane Akt inhibitors.

Array Biopharma

Non-oxime inhibitors of B-Raf(V600E) kinase.

Array Biopharma

Discovery of dihydrothieno- and dihydrofuropyrimidines as potent pan Akt inhibitors.

Array Biopharma

Discovery of pyrrolopyrimidine inhibitors of Akt.

Array Biopharma

Prodrug thiamine analogs as inhibitors of the enzyme transketolase.

Array Biopharma

Tetrazole and ester substituted tetrahydoquinoxalines as potent cholesteryl ester transfer protein inhibitors.

Array Biopharma

Potent and selective mitogen-activated protein kinase kinase (MEK) 1,2 inhibitors. 1. 4-(4-bromo-2-fluorophenylamino)-1- methylpyridin-2(1H)-ones.

Array Biopharma

Discovery and SAR of trisubstituted thiazolidinones as CCR4 antagonists.

Array Biopharma

Discovery and preclinical development of AR453588 as an anti-diabetic glucokinase activator.

Array Biopharma

Identification of the Clinical Development Candidate

Array Biopharma

Discovery of (S)-1-(1-(4-Chloro-3-fluorophenyl)-2-hydroxyethyl)-4-(2-((1-methyl-1H-pyrazol-5-yl)amino)pyrimidin-4-yl)pyridin-2(1H)-one (GDC-0994), an Extracellular Signal-Regulated Kinase 1/2 (ERK1/2) Inhibitor in Early Clinical Development.

Array Biopharma

Discovery of Tetrahydropyridopyrimidines as Irreversible Covalent Inhibitors of KRAS-G12C with In Vivo Activity.

Array Biopharma

Highly potent and selective 3-N-methylquinazoline-4(3H)-one based inhibitors of B-Raf(V600E) kinase.

Array Biopharma

Discovery of danoprevir (ITMN-191/R7227), a highly selective and potent inhibitor of hepatitis C virus (HCV) NS3/4A protease.

Array Biopharma

Imidazo[4,5-b]pyridine inhibitors of B-Raf kinase.

Array Biopharma

Pyrazolopyridine inhibitors of B-Raf(V600E). Part 4: rational design and kinase selectivity profile of cell potent type II inhibitors.

Array Biopharma

Potent and selective pyrazolo[1,5-a]pyrimidine based inhibitors of B-Raf(V600E) kinase with favorable physicochemical and pharmacokinetic properties.

Array Biopharma

The discovery of potent and selective pyridopyrimidin-7-one based inhibitors of B-RafV600E kinase.

Array Biopharma

Pyrazolopyridine Inhibitors of B-Raf(V600E). Part 1: The Development of Selective, Orally Bioavailable, and Efficacious Inhibitors.

Array Biopharma

Pyrazolopyridine inhibitors of B-Raf(V600E). Part 3: an increase in aqueous solubility via the disruption of crystal packing.

Array Biopharma

ISOINDOLINES AS PMS2 INHIBITORS

Neophore

Imidazopyridazine compounds and uses thereof

Incyte

Pyrazine derivative and application thereof in inhibiting SHP2

Suzhou Genhouse Pharmaceutical

Pyridone amides as modulators of sodium channels

Vertex Pharmaceuticals

Diazaindole derivative and use thereof as CHK1 inhibitor

Medshine Discovery

Indole carboxamide compounds

Bristol-Myers Squibb

Certain chemical compositions and methods of use thereof

Algen Biotechnologies

CIS-morpholinone and other compounds as MDM2 inhibitors for the treatment of cancer

Amgen

Selective inhibitors of protein arginine methyltransferase 5 (PRMT5)

Prelude Therapeutics

Dipeptidyl ketoamide meta-methoxyphenyl derivatives and uses thereof

Landsteiner Genmed

Pyrrolopyrimidine and pyrrolopyridine derivatives

Galapagos

Diazabicyclic substituted imidazopyrimidines and their use for the treatment of breathing disorders

Bayer Aktiengesellschaft

Cyclic dinucleotides as sting agonists

Janssen Biotech

Compounds and uses thereof

Kala Pharmaceuticals

Beta adrenergic agonist and methods of using the same

Curasen Therapeutics

Cannabinergic compounds and uses thereof

Northeastern University

Heteroaromatic compounds as BTK inhibitors

Boehringer Ingelheim International

HDAC inhibitors for the treatment of diabetic peripheral neuropathy

Regenacy Pharmaceuticals

2-(morpholin-4-yl)-1,7-naphthyridines

Bayer Pharma Aktiengesellschaft

2-(pyrazolopyridin-3-yl)pyrimidine derivatives as JAK inhibitors

Almirall

Heteroaryl-substituted sulfonamide compounds and their use as sodium channel inhibitors

Xenon Pharmaceuticals

Benzimidazole derivatives as EP4 ligands

Bayer Pharma Aktiengesellschaft

Heterocyclic compounds for the treatment of disease

Oppilan Pharma

Substituted imidazo[1,2-a]pyridines as PDE-10 inhibitors

Sunovion Pharmaceuticals

TYK2 inhibitors and uses thereof

Nimbus Lakshimi

Fused amino pyridine as HSP90 inhibitors

Curis

1-(3-aminopropyl) substituted cyclic amine compounds, preparation method therefor, and pharmaceutical compositions and uses thereof

Shanghai Institute of Material Medica, Chinese Academy of Sciences

Pyrrole six-membered heteroaryl ring derivative, preparation method thereof, and medicinal uses thereof

Jiangsu Hengrui Medicine

Cyclopentylbenzamide derivatives and their use for the treatment of psychotic and cognitive disorders

Takeda Pharmaceutical

Inhibitors of matrix metalloproteinases

Pharmahungary 2000

6-alkynyl-pyridine derivatives

Boehringer Ingelheim International

Synthesis of a novel series of L-isoserine derivatives as aminopeptidase N inhibitors.

Shandong University

Synthesis and biological evaluation of novel N,N'-bis-methylenedioxybenzyl-alkylenediamines as bivalent anti-Alzheimer disease ligands.

Sun Yat-Sen University

Compounds

Respivert

Aminopyrimidine derivatives for use as modulators of kinase activity

Merck Patent

Tetracyclic CDK9 kinase inhibitors

Abbvie

Small-Molecule Inhibitors of the SOX18 Transcription Factor.

The University of Queensland

Pyrazole and imidazole derivatives useful as orexin antagonists

Actelion Pharmaceuticals

Heterocyclyl aminoimidazopyridazines

Bayer Intellectual Property

Pyridinones/pyrazinones, method of making, and method of use thereof

Genentech

6-thio-substituted imidazo[1,2-a]pyrazines as Mps-1 inhibitors

Bayer Intellectual Property

Substituted pyrimidine compounds and their use as SYK inhibitors

Genosco

Methods and compositions for studying, imaging, and treating pain

The Leland Stanford Junior University

Inhibitor Discovery for the Human GLUT1 from Homology Modeling and Virtual Screening.

Icahn School of Medicine At Mount Sinai

Tricyclic triazole compounds that modulate HSP90 activity

Synta Pharmaceuticals

Chemical compounds

Astrazeneca

Radiolabeled PDE10A ligands

Abbvie

Solid forms of gyrase inhibitor (R)-1-ethyl-3-[6-fluoro-5-[2-(1-hydroxy-1-methyl-ethyl)pryimidin-5-yl]-7-(tetrahydrofuran-2-yl)-1H-benzimidazol-2-yl]urea

Vertex Pharmaceuticals

Repurposing human PDE4 inhibitors for neglected tropical diseases. Evaluation of analogs of the human PDE4 inhibitor GSK-256066 as inhibitors of PDEB1 of Trypanosoma brucei.

Northeastern University

4-(azacycloalkyl)benzene-1,3-diol compounds as tyrosinase inhibitors, process for the preparation thereof and use thereof in human medicine and in cosmetics

Galderma Research & Development

Discovery of novel tricyclic pyrido[3',2':4,5]thieno[3,2-d]pyrimidin-4-amine derivatives as VEGFR-2 inhibitors.

Suez Canal University

Ring-substituted N-pyridinyl amides as kinase inhibitors

Novartis

Solid-phase synthesis of a combinatorial array of 1,3-bis(acylamino)-2-butanones, inhibitors of the cysteine proteases cathepsins K and L.

Smithkline Beecham Pharmaceuticals

Inhibition of forskolin-induced neurite outgrowth and protein phosphorylation by a newly synthesized selective inhibitor of cyclic AMP-dependent protein kinase, N-[2-(p-bromocinnamylamino)ethyl]-5-isoquinolinesulfonamide (H-89), of PC12D pheochromocytoma cells.

Nagoya University School of Medicine

Synthesis and in vivo evaluation of a novel 5-HT1A receptor agonist radioligand [O-methyl- 11C]2-(4-(4-(2-methoxyphenyl)piperazin-1-yl)butyl)-4-methyl-1,2,4-triazine-3,5(2H,4H)dione in nonhuman primates.

Columbia University

A structure/activity relationship study on arvanil, an endocannabinoid and vanilloid hybrid.

Istituto Di Chimica Biomolecolare

SAR of carbon-linked, 2-substituted purines: synthesis and characterization of AP23451 as a novel bone-targeted inhibitor of Src tyrosine kinase with in vivo anti-resorptive activity.

Ariad Pharmaceuticals

The discovery of novel vascular endothelial growth factor receptor tyrosine kinases inhibitors: pharmacophore modeling, virtual screening and docking studies.

Shanghai Jiao Tong University

A structure-guided approach to creating covalent FGFR inhibitors.

Harvard Medical School

Rational design, synthesis, and biological evaluation of progesterone-modified MRI contrast agents.

Northwestern University

Structure-based design of potent and selective cell-permeable inhibitors of human beta-secretase (BACE-1).

Merck Research Laboratories